| ObjectiveTo develop novel type of transdermal delivery system-cataplasm by reforming the formulation of Hongzhi Guke powder which is a kind of pharmaceutics for medical institutes, according to the factors such as drug administering characteristics and administration route of original formula. To meet the clinical demands, to make traditional Chinese medicine(TCM) give full play in the treatment of orthopedic diseases and to offer some reference for research and development of TCM topical preparations by preparing a sort of cataplasm which is safe, effective, comfortable and convenient.Methods1. By consulting relevant literature and some exploration, the matrix type and scope, the shaping conditions and the preparation technology were preliminary determined. The shaping technology was optimized by orthogonal experiment, providing the reference for the batch production of Hongzhi Gutong cataplasm. The orthogonal test method was used to optimize the optimal formulation of Hongzhi Gutong cataplasm. Then for laboratory small batch production, the result showed that the process is stable and reliable.2. According to the cataplasm inspection items and methods recorded in the Chinese Pharmacopoeia (2010, part one)appendix Ⅱ, the quality of Hongzhi Gutong cataplasm was evaluated, qualitative identification of Phellodendron, Rhubarb and Chinese Starjasmine Stem in the cataplasm was carried out by TLC, meanwhile, HPLC was used to determine the content of Gardenin and berberine hydrochloride and methodologically inspected.3. According to technical requirements related guidance technology principles of stability test of raw medicine and pharmaceutical preparations recorded in the Chinese Pharmacopoeia (2010, part two)appendix Ⅺ, X c, Hongzhi Gutong cataplasm was studied by Accelerated stability test and long-term stability; according to the technical guiding principles of irritant and hemolytic study on TCM and natural medicine, the skin irritation for New Zealand rabbits was investigated.Results1. The optimal substrate materials, reasonable consumption and stable processing technique was established by constantly exploring and lots of practice. When the NP-800 dosage of 0.8～1.6g (4.3%-8.6%) would be better at 1.0-1.4g (5.4%～8.6%); aluminum glycinate at 0.04～1.0g(0.2%～5.4%); the amount of tartaric acid 0.01～0.06g (0.05%～0.3%); glycerol 4-8g (21.6%-43.2%), more reasonable at 5～6g (27%～32.4%); PVP-K90 0.1～0.8g (0.5%～4.3%), far more superior to that at 0.2～0.4g (1.0%～2.1%). As for the stable processing technique we found that the influence of the standing and solidifying conditions of the cataplasm on the shape of it was remarkable, which when the temperature was about 30℃ and the relative humidity was about 60%. The optimal ratio prescription of Hongzhi Gutong cataplasm was as follows: NP-800-aluminum glycinate-glycerol-PVP K 90(1.2:0.04:6:0.4). Thus, the final preparation process established:Weighing the prescribed amount of NP-800, aluminum glycinate dispersed in glycerol as oil phase, the aqueous solution of tartaric acid, PVP-K90 as well of the herbal extract added into the oil phase above, and then stirred it to be pasty, applied it to a non-woven fabric, covered it with release film, and then made it stand to be a shape.2. TLC was used to idengtify Phellodendron, Rhubarb and Chinese Star jasmine Stem in the cataplasm, the separation was good, clear spots, and negative control without interference. The results indicated that the amount of ointent was no less than 16g per 100cm2; early viscous force test showed that it can stick on the 17th ball, lasting viscous force test time should be more than 160s. Shaping, heat resistance, microbial limits and so on meet the requirements of Chinese pharmacopoeia. Each piece of the Hongzhi Gutong cataplasm must contain no less than 5.5mg berberine hydrochloride and at least 1.8mg Garden in.3. The results of the Accelerated stability test and Long-Term stability showed that the stability of the Hongzhi Gutong cataplasm was good. And the outcome of the Skin irritation test indicated that this cataplasm has no acute toxicity reaction when applied to the normal and wounded skin in New Zealand rabbit body. ConclusionThe prescription of Hongzhi Gutong cataplasm developed by this study is reasonably practicable. It can be used as reference for other external preparation of Chinese medicine. It comes up with the standard quality and meets the requirements of the pharmacopoeia. It is safe and has good effects. It is has a good prospecting. |
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